The preparation of novel PET radiopharmaceuticals is dependent on the availability of methods to incorporate the desired radioisotope into the scaffold of interest. Many interesting potential PET imaging agents cannot be investigated or prepared for clinical use as they cannot be accessed by existing methods in good reproducible yields. There has been significant advancement in fluorination methods for late-stage fluorine-18 radiolabeling of bioactive molecules and drug scaffolds. Metal-mediated reactions with fluorine-18 are one such advancement, which in a relatively short period of time have changed the way radiochemists form C-18F bonds, revolutionizing the PET radiochemistry landscape. A wide range of substrates have been utilized in these reactions to enable the radiofluorination of novel and previously difficult or impossible to prepare radiopharmaceuticals using traditional fluorine-18 radiochemistry. In addition, our laboratory has looked at the formulation of cyclotron produced fluorine-18 into different fluoride reagents to allow investigation of additional fluoride methodology with fluorine-18, which has not yet been explored in radiochemistry due to previous difficulties in the preparation of such fluoride reagents, including Ag-18F. This presentation will cover our laboratory’s recent progress developing reactions that convert C–B, C–Sn and C-H bonds into C–18F bonds using readily available high specific activity nucleophilic fluoride.

Transition-metal mediated late-stage radiofluorination

255th National Meeting (2018)

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